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S1RA | Selective sigma-1 antagonist

S1RA (E-52862, 1265917-14-3) is a potent and selective σ1 antagonist with weak binding at σ2 (IC50 σ1 = 17nM, σ2 = 9300nM).1,2 S1RA abolished mechanical and thermal hyperalgesia in mice with carrageenan-induced acute inflammation by enhancing the action of endogenous opioid peptides of immune origin in a σ1 dependent manner.3 BD1063 potentiated µ-opioid antinociception in mice in a σ-dependent manner.4 S1RA displayed neuroprotective effects in a mouse model of ischemic stroke.5



1) Romero et al. (2012), Pharmacological properties of S1RA, a new sigma-1 receptor antagonist that inhibits neuropathic pain and activity-induced spinal sensitization; Br. J. Pharmacol. 166 2289
2) Diaz et al. (2012), Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-Methyl-1-(napthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine hydrochloride (S1RA, E-52862); J. Med. Chem. 55 8211
3) Tejada et al. (2017), Sigma-1 receptors control immune-driven peripheral opioid analgesia during inflammation in mice; Proc. Natl. Acad. Sci. USA 114 8396
4) Sanchez-Fernandez et al. (2014), Modulation of peripheral μ-opioid analgesia by σ1 receptors; J. Pharmacol. Exp. Ther. 348 32
5) Sanchez-Blazquez et al. (2018), The Sigma-1 Receptor Antagonist, S1RA, Reduces Stroke Damage, Ameliorates Post-Stroke Neurological Deficits and Suppresses the Overexpression of MMP-9; Mol. Neurobiol. 55 4940

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Catalog#  10-4201-0005

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Catalog Number:
Selective Sigma1 agonist
Chemical Name:
4-{2-[5-Methyl-1-(napthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine hydrochloride
Alternate Names:
E-52862 HCl
Molecular Weight:
Molecular Formula:
C20H23N3O2 • HCl
Soluble in DMSO (up to at least 25 mg/ml)
Physical Properties:
Off-white solid
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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